Drug intelligence / Profile preview

213Bi-DOTA-biotin

Development stage
Preclinical
Lead developer
National Institutes of Health
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

**213Bi-DOTA-biotin** is a radiopharmaceutical compound used in pretargeted radioimmunotherapy, particularly for cancer. It consists of the alpha-emitting radionuclide **Bismuth-213 (213Bi)** chelated to biotin via the macrocyclic chelator DOTA (1,4,7,10-tetraazacyclododecane-N,N',N",N'"-tetraacetic acid). In therapy, an antibody-streptavidin conjugate is administered to the patient to target specific tumor antigens, followed by a clearing agent and then the injection of 213Bi-DOTA-biotin; the biotin binds tightly to the tumor-localized streptavidin, delivering high-energy, short-range alpha radiation that destroys tumor cells. This approach enhances tumor specificity and minimizes damage to surrounding healthy tissue. The mechanism relies on cell-killing DNA damage induced by alpha particles. Preclinical studies have demonstrated effectiveness in models of adult T-cell leukemia and solid tumors, but optimal use is limited by renal toxicity and a low therapeutic index. Primary research developers and specific manufacturers are not uniquely established entities, but research has involved institutions such as the National Institutes of Health and various academic collaborations[1][2][3][4][5][6].

Other names
Bismuth-213-DOTA-biotinBismuth213-DOTA-biotinBismuth 213-DOTA-biotin
02

Targets

DNA

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